Enzymatic synthesis of [4-methoxy-11C]daunorubicin for functional imaging of P-glycoprotein with PET
| Autor: | Philippus Elsinga, W Vaalburg, E Eriks-Fluks, NH Hendrikse, Ejf Franssen |
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| Přispěvatelé: | Clinical pharmacology and pharmacy |
| Rok vydání: | 1998 |
| Předmět: |
Stereochemistry
Daunorubicin Methylation chemistry.chemical_compound medicine ATP Binding Cassette Transporter Subfamily B Member 1 Carbon Radioisotopes P-glycoprotein chemistry.chemical_classification Radiation Methionine biology Carubicin Total synthesis Multiple drug resistance Enzyme chemistry Biochemistry Isotope Labeling biology.protein Radiopharmaceuticals Tomography Emission-Computed Methyl iodide medicine.drug |
| Zdroj: | Eriks-Fluks, E, Elsinga, P H, Hendrikse, N H, Franssen, E J F & Vaalburg, W 1998, ' Enzymatic synthesis of [4-methoxy-11 C]daunorubicin for functional imaging of P-glycoprotein with PET ', Applied Radiation and Isotopes, vol. 49, no. 7, pp. 811-813 . https://doi.org/10.1016/S0969-8043(97)00302-3 Applied Radiation and Isotopes, 49(7), 811-813. Elsevier Limited |
| ISSN: | 0969-8043 |
| DOI: | 10.1016/s0969-8043(97)00302-3 |
| Popis: | One of the mechanisms for multidrug resistance (MDR) of tumors is an overexpression of the P-glycoprotein (P-gp). The cytostatic agent daunorubicin was labeled with carbon-11 to probe P-gp with PET. An enzymatic route for the conversion of carminomycin to [4-methoxy-11C]daunorubicin ([4-methoxy-11C]DNR) was investigated, since attempts failed to prepare daunorubicin chemically using [11C]methyl iodide. In the enzymatic synthesis methylation was accomplished by S-adenosyl-L-[methyl- 11C]methionine ([11]SAM), which was synthesized from L-[methyl- 11C]methionine. This methylation is catalyzed by carminomycin-4-O- methyltransferase (CMT). The overall radiochemical yield of [4- methoxy.11C]DNR is 1% (EOB), with a total synthesis time of 75 min. In conclusion, [4-methoxy-11C]DNR can be successfully prepared from carminomycin and [11C]SAM using enzymes. |
| Databáze: | OpenAIRE |
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